eTFC-01:一个双标记的酸盐桥接标志物用于SSTR2-阳性瘤
Dylan Chapeau1,2, Savanne Beekman1,2, Maryana Handula1,2
1Erasmus MC, Department of Radiology and Nuclear Medicine, University Medical Center Rotterdam, Rotterdam, The Netherlands.
EJNMMI radiopharmacy and chemistry
|May 22, 2024
概括
研究人员开发了一种新型的三功能酸盐,用于双重放射性和光学成像追踪器. 虽然体外结果是有希望的,但体内研究显示瘤吸收率较低,并建议进行修改,以改善标记物分布.
科学领域:
- 生物医学成像技术 生物医学成像技术
- 放射化学 放射化学是指辐射化学.
- 分子成像学分子成像学
背景情况:
- 整合放射性和光学成像可以提高癌症患者的预后和外科指导.
- 双标记的标记剂提供一致性,但由于硬质障碍,其开发具有挑战性.
- 一种新的三功能酸盐被设计为在相反的位置配对光染料和向载体,从而最大限度地减少硬质障碍.
研究的目的:
- 合成和评估一种用于双标签成像追踪器的新型三功能酸盐.
- 评估双标记标记器ETFC-01.1的体外和体内性能.
主要方法:
- 通过五步路径合成了一种三功能酸盐 (N3-Py-DOTAGA-(tBu) 3).
- 使用固相合成将酸盐结合为线性,然后进行脱保护和循环.
- 引入近红外光染料 (sulfo-Cy.5) 使用无铜点击化学,创建ETFC-01,并标记为111In.
主要成果:
- 与DOTA-TATE相比,eTFC-01显示SSTR2的IC50是SSTR2的两倍.
- [111In]In-eTFC-01标签实现了高放射性化学产量和纯度.
- [111In]-eTFC-01的细胞吸收量在体外是[111In]-eTFC-01的两倍低于[111In]-DOTA-TATE;体内瘤吸收量也较低,在高度血管化的组织中积累增加.
结论:
- 三功能酸盐方法可用于创建双标记的标记物.
- 试验室结果很有希望,但[111In]In-eTFC-01的体内性能表明需要优化以改善瘤向和分布.
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